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公开(公告)号：US07345083B2
公开(公告)日：2008-03-18
申请号：US11714352
申请日：2007-03-06
IPC分类号： A61K31/4035 , C07D209/44
CPC分类号： C07D209/44
摘要： The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
摘要翻译： 本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的某些加氢异吲哚啉化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂和 使用化合物及其制剂治疗某些疾病，包括呕吐，尿失禁，抑郁和焦虑。
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公开(公告)号：US07645790B2
公开(公告)日：2010-01-12
申请号：US10586727
申请日：2005-01-26
IPC分类号： A61K31/4035 , C07D209/44
CPC分类号： C07D209/44
摘要： The present invention is directed to certain hydroisoindoline compounds of formula I which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
摘要翻译： 本发明涉及某些可用作神经激肽-1（NK-1）受体拮抗剂和速激肽抑制剂，特别是物质P的式I的加氢异吲哚啉化合物。本发明还涉及包含这些化合物作为活性的药物制剂 成分以及化合物及其制剂在治疗某些疾病（包括呕吐，尿失禁，抑郁和焦虑）中的用途。
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公开(公告)号：US20080280966A1
公开(公告)日：2008-11-13
申请号：US10586727
申请日：2005-01-26
IPC分类号： A61K31/403 , C07D209/44
CPC分类号： C07D209/44
摘要： The present invention is directed to certain hydroisoindoline compounds of formula I which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
摘要翻译： 本发明涉及某些可用作神经激肽-1（NK-1）受体拮抗剂和速激肽抑制剂，特别是物质P的式I的加氢异吲哚啉化合物。本发明还涉及包含这些化合物作为活性的药物制剂 成分以及化合物及其制剂在治疗某些疾病（包括呕吐，尿失禁，抑郁和焦虑）中的用途。
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公开(公告)号：US07217731B2
公开(公告)日：2007-05-15
申请号：US11043213
申请日：2005-01-26
IPC分类号： A61K31/4035 , C07D209/44
CPC分类号： C07D209/44
摘要： The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
摘要翻译： 本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的某些加氢异吲哚啉化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂和 使用化合物及其制剂治疗某些疾病，包括呕吐，尿失禁，抑郁和焦虑。
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公开(公告)号：US07683068B2
公开(公告)日：2010-03-23
申请号：US11920286
申请日：2006-06-23
IPC分类号： A61K31/497 , A61K31/4035 , A61K31/4439 , C07D209/46 , C07D405/04 , C07D409/04 , A61P29/00
CPC分类号： C07D209/46 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
摘要翻译： 本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的某些加氢异吲哚啉化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂和 使用化合物及其制剂治疗某些疾病，包括呕吐，尿失禁，抑郁和焦虑。
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公开(公告)号：US20090054462A1
公开(公告)日：2009-02-26
申请号：US11920286
申请日：2006-06-23
IPC分类号： A61K31/497 , C07D209/46 , C07D405/04 , C07D409/04 , A61K31/4035 , A61P29/00 , A61P11/00 , A61P13/00 , A61P1/00 , A61P25/00 , A61K31/4439 , C07D401/04 , C07D403/04
CPC分类号： C07D209/46 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
摘要翻译： 本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的某些加氢异吲哚啉化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂和 使用化合物及其制剂治疗某些疾病，包括呕吐，尿失禁，抑郁和焦虑。
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公开(公告)号：US20090253673A1
公开(公告)日：2009-10-08
申请号：US12227545
申请日：2007-07-06
申请人： Min Ge , Eric Cline , Lihu Yang , Sander G. Mills
发明人： Min Ge , Eric Cline , Lihu Yang , Sander G. Mills
IPC分类号： A61K31/4155 , C07D403/06 , C07D401/06 , C07D231/12 , C07D231/38 , C07D413/12 , C07D417/12 , A61K31/415 , A61K31/454 , A61K31/496 , A61K31/4178 , A61K31/422 , A61K31/4245 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/427 , A61P3/04 , A61P3/10
CPC分类号： C07D403/12 , C07D231/38 , C07D401/06 , C07D401/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： Certain novel N-acylated spiropiperidine derivatives are ligands of the human ghrelin receptor(s) and, in particular, are antagonists/inverse agonists of the human ghrelin receptor. They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of the ghrelin receptor, such as obesity, diabetes, and metabolic syndrome.
摘要翻译： 某些新的N-酰化螺哌啶衍生物是人类生长素释放肽受体的配体，特别是人类生长素释放肽受体的拮抗剂/反向激动剂。 因此，它们可用于治疗，控制或预防响应于调节生长素释放肽受体的疾病和病症，例如肥胖，糖尿病和代谢综合征。
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18.发明授权Tetrahydropyranyl cyclopentyl tetrahydropyridopyridine modulators of chemokine receptor activity 失效趋化因子受体活性的四氢吡喃基环戊基四氢吡啶并吡啶调节剂公开(公告)号：US07557124B2
公开(公告)日：2009-07-07
申请号：US11587288
申请日：2005-04-22
申请人： Lihu Yang , Sander G. Mills , Richard Jiao
发明人： Lihu Yang , Sander G. Mills , Richard Jiao
IPC分类号： C07D405/02 , C07D309/14 , A61K31/47 , A61K31/351
CPC分类号： C07D309/14 , C07D405/12
摘要： Compounds of Formula I: (wherein n, R1, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.
摘要翻译： 式I化合物（其中n，R 1，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 15，R 16，Y和Z如本文所定义），其是趋化因子受体活性的调节剂， 预防或治疗某些炎性和免疫调节性疾病和疾病，过敏性疾病，特应性病症，包括过敏性鼻炎，皮炎，结膜炎和哮喘，以及自身免疫病态如类风湿性关节炎和动脉粥样硬化。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及趋化因子受体的疾病中的用途。
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公开(公告)号：US07091211B2
公开(公告)日：2006-08-15
申请号：US10901414
申请日：2004-07-28
申请人： Paul E. Finke , Jennifer L. Loebach , Kerry A. Parker , Christopher W. Plummer , Sander G. Mills
发明人： Paul E. Finke , Jennifer L. Loebach , Kerry A. Parker , Christopher W. Plummer , Sander G. Mills
IPC分类号： A61K31/438 , C07D401/04
CPC分类号： C07D471/10 , C07D471/20 , C07D491/10 , C07D491/20 , C07D498/10
摘要： Cyclopentyl compounds of Formula (I) are modulators of chemokine receptor activity: wherein D, G, R2, R3 and R8 in Formula (I) are defined herein. The compounds, and pharmaceutically acceptable salts and individual diastereomers thereof, are useful in the treatment and prevention of HIV infection, in delaying the onset of AIDS, and in the treatment of AIDS. The compounds are also useful for treating other diseases and conditions mediated by chemokine receptors.
摘要翻译： 式（I）的环戊基化合物是趋化因子受体活性的调节剂：其中式（I）中的D，G，R 2，R 3和R 8 （I）在本文中定义。 化合物及其药学上可接受的盐和单独的非对映异构体可用于治疗和预防艾滋病毒感染，延缓艾滋病的发病和艾滋病的治疗。 该化合物也可用于治疗趋化因子受体介导的其它疾病和病症。
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公开(公告)号：US06638930B2
公开(公告)日：2003-10-28
申请号：US09836716
申请日：2001-04-17
申请人： Conrad P. Dorn , Paul E. Finke , Jeffrey J. Hale , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian John Williams
发明人： Conrad P. Dorn , Paul E. Finke , Jeffrey J. Hale , Malcolm Maccoss , Sander G. Mills , Shrenik K. Shah , Mark Stuart Chambers , Timothy Harrison , Tamara Ladduwahetty , Brian John Williams
IPC分类号： A61K315377
CPC分类号： A61K31/41 , A61K31/50 , A61K31/53 , A61K31/535 , A61K31/54 , C07D265/30 , C07D265/32 , C07D279/12 , C07D413/04 , C07D413/06 , C07D413/14 , Y10S514/872
摘要： Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
摘要翻译： 取代的通式结构式的杂环是用于治疗炎性疾病，疼痛或偏头痛，哮喘和呕吐的速激肽受体拮抗剂，以及可用于治疗心血管疾病如心绞痛，高血压或缺血的钙通道阻滞剂。
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